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Alexander Jetter et al.
European journal of clinical pharmacology, 60(3), 165-171 (2004-03-27)
The hypoglycaemic drug tolbutamide is used for assessment of CYP2C9 activity in vivo. However, therapeutically active doses of 500 mg bear the risk of hypoglycaemia, and a tolbutamide-derived parameter based on a single plasma or urine concentration reflecting CYP2C9 activity
Impaired (S)-warfarin metabolism catalysed by the R144C allelic variant of CYP2C9.
A E Rettie et al.
Pharmacogenetics, 4(1), 39-42 (1994-02-01)
J Karbwang et al.
The Southeast Asian journal of tropical medicine and public health, 19(2), 235-241 (1988-06-01)
The effects of mefloquine (MQ), the combination of MQ with sulfadoxine-pyrimethamine (MSP), sulfadoxine (S), pyrimethamine (P) quinine (Q) and quinidine (Qd) on in vitro hepatic metabolism has been studied using tolbutamide as a substrate. The hydroxylation of tolbutamide was determined
Use of tolbutamide as a substrate probe for human hepatic cytochrome P450 2C9.
J O Miners et al.
Methods in enzymology, 272, 139-145 (1996-01-01)
A K Miller et al.
European journal of clinical pharmacology, 38(5), 523-524 (1990-01-01)
Tolbutamide (1 g/70 kg) was administered as a single intravenous dose to 31 healthy, non-smoking, drug-free males between 23 and 87 years old and the total amounts of hydroxy and carboxytolbutamide excreted in 24 h were measured. There was a
An HPLC method for the simultaneous determination of tolbutamide and its metabolites in plasma.
P Pecorari et al.
Il Farmaco; edizione pratica, 36(1), 7-12 (1981-01-01)
D J Back et al.
British journal of pharmacology, 85(1), 121-126 (1985-05-01)
Tolbutamide has been used as a model drug for an examination of the effects of eleven substituted imidazole compounds on hepatic metabolism in vivo. The 1-substituted compounds 1-methylimidazole, miconazole, clotrimazole and ketoconazole produced marked alterations in tolbutamide kinetics (increased half-life
Soo Hyeon Bae et al.
Antimicrobial agents and chemotherapy, 58(9), 5036-5046 (2014-06-04)
Macrolactin A (MA) and 7-O-succinyl macrolactin A (SMA), polyene macrolides containing a 24-membered lactone ring, show antibiotic effects superior to those of teicoplanin against vancomycin-resistant enterococci and methicillin-resistant Staphylococcus aureus. MA and SMA are currently being evaluated as antitumor agents
Jang Su Jeon et al.
Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association, 76, 94-102 (2014-12-24)
meso-Dihydroguaiaretic acid (MDGA) is a major component of Myristica fragrans and Machilus thunbergii that is traditionally used as a spice and for medicinal purposes. Despite reports of various biological activities exerted by MDGA, there is no information regarding its metabolic
P Dogterom et al.
Drug metabolism and disposition: the biological fate of chemicals, 21(4), 705-709 (1993-07-01)
Precision-cut liver slices from rats and dogs were used to investigate in vitro the metabolism of tolbutamide. Tolbutamide (100 microM) was incubated with liver slices in 12-well plates (rat: 1 slice/well; dog: 4 slices/well) for up to 9 hr. In
Biotransformation of tolbutamide to 4'-hydroxytolbutamide by the fungus Cunninghamella blakesleeana.
Haihua Huang et al.
Applied microbiology and biotechnology, 72(3), 486-491 (2006-02-24)
The hypoglycemic drug tolbutamide is commonly used as a probe drug to evaluate CYP2C9 enzyme activity in terms of production of 4'-hydroxytolbutamide. In the present study, an initial screening of seven filamentous fungi was carried out to identify which was
In vitro and in vivo characterization of 13 CYP2C9 allelic variants found in Chinese Han population.
Guo-Xin Hu et al.
Drug metabolism and disposition: the biological fate of chemicals, 43(4), 561-569 (2015-01-24)
Our previous study detected totally 35 CYP2C9 allelic variants in 2127 Chinese subjects, of whom 21 novel alleles were reported for the first time in Chinese populations. The aim of the present study was to characterize the 13 CYP2C9 allelic
Shun-Bin Luo et al.
Journal of pharmacological sciences, 125(2), 150-156 (2014-07-31)
Warfarin is the most frequently prescribed anticoagulant for the long-term treatment in the clinic. Recent studies have shown that polymorphic alleles within the CYP2C9, VKORC1, and CYP4F2 genes are related to the warfarin dosage requirement. In this study, a novel
Cuyue Tang et al.
Drug metabolism and disposition: the biological fate of chemicals, 30(6), 648-654 (2002-05-23)
The cytochrome P450 (P450)-dependent conversion of phenytoin (PHT) to p-hydroxy phenytoin (pHPPH), and tolbutamide (TLB) to 4-hydroxy tolbutamide (hydroxy-TLB), in human liver microsomes was studied in the presence of increasing concentrations (0-4%) of bovine serum albumin (BSA). Therefore, the free
Chunhuan Jin et al.
Xenobiotica; the fate of foreign compounds in biological systems, 45(7), 571-577 (2015-03-27)
1. The present study was conducted to examine the possibility of herb-drug interaction by celastrol, which is a main compound isolated from Tripterygium wilfordii Hook F. using human liver microsomes with cocktail methods. Focused on its inhibitory manner on the metabolism
Y K Leung et al.
Journal of biochemical and biophysical methods, 36(2-3), 87-94 (1998-08-26)
A simple HPLC/fluorescence method to detect hydroxytolbutamide (a major metabolite of the anti-diabetic drug tolbutamide) has been developed. The effects of nicotine and some of its metabolites on tolbutamide hydroxylation is described. An extraction procedure with diethyl ether was followed
Ji-Hong Shon et al.
Pharmacogenetics, 12(2), 111-119 (2002-03-05)
Several recent in-vitro data have revealed that CYP2C19, in addition to CYP2C9, is also involved in the 4-methylhydroxylation of tolbutamide. We evaluated the relative contribution of CYP2C9 and CYP2C19 genetic polymorphisms on the disposition of blood glucose lowering response to
Simultaneous determination of tolbutamide and its hydroxy and carboxy metabolites in plasma and urine by high-performance liquid chromatography.
J Keal et al.
Journal of chromatography, 378(1), 237-241 (1986-05-28)
S St-Hilaire et al.
Journal of pharmaceutical sciences, 78(10), 863-866 (1989-10-01)
Methods of analysis of tolbutamide (1) and its hydroxylated (2) and carboxylated (3) metabolites in serum and urine based on high-performance liquid chromatography were developed. The separation was performed on a Apex ODS column in the isocratic mode using a
A S Gross et al.
British journal of clinical pharmacology, 47(2), 151-156 (1999-04-06)
Ethnic differences in drug disposition have been described for many drugs. Despite the widespread use of tolbutamide in Asian populations, the pharmacokinetics of tolbutamide, a CYP2C9 substrate, have not been described in ethnic Chinese. The pharmacokinetics of tolbutamide (500 mg
Julia Kirchheiner et al.
Pharmacogenetics, 12(2), 101-109 (2002-03-05)
Tolbutamide is known to be metabolized by cytochrome P450 2C9 (CYP2C9), and the effects of the CYP2C9 amino acid polymorphisms *2 (Arg144Cys) and *3 (Ile359Leu) could be important for drug treatment with tolbutamide and for use of tolbutamide as a
K Washio et al.
The Journal of pharmacy and pharmacology, 45(3), 231-233 (1993-03-01)
We investigated the metabolism of tolbutamide by using synthetic 1-butyl-3-(p-formylphenyl)sulphonylurea (ATB), an intermediate in the metabolic pathway of tolbutamide. ATB (40 mg kg-1) administered intravenously to rabbits was oxidized to 1-butyl-3-(p-carboxyphenyl)sulphonylurea (CTB) and also reduced to 1-butyl-3-(p-hydroxymethylphenyl)sulphonylurea (HMTB). Therefore, it
D J Back et al.
British journal of pharmacology, 81(3), 557-562 (1984-03-01)
The effects of various drugs on the pharmacokinetics of tolbutamide have been examined in the rat. Phenobarbitone pretreatment caused a significant decrease in half life and area under the curve (AUC) and a significant increase in clearance and volume of
Sang Yoon Lee et al.
Toxicology letters, 229(1), 33-40 (2014-06-10)
Although cytochrome P450 inhibition is the major drug-drug interaction (DDI) mechanism in clinical pharmacotherapy, DDI of a number of well-established drugs have not been investigated. Rifampicin, isoniazid, pyrazinamide and ethambutol combination therapy inhibits clearance of theophylline in patients with tuberculosis.
M E Veronese et al.
Pharmacogenetics, 3(2), 86-93 (1993-04-01)
The tolbutamide hydroxylation capacity was studied in 106 healthy unrelated volunteers from the Australian population. Following a 500 mg oral dose of tolbutamide, the ratio of metabolites (hydroxytolbutamide plus carboxytolbutamide) to unchanged tolbutamide excreted in urine from 6 to 12
M E Veronese et al.
Clinical pharmacology and therapeutics, 47(3), 403-411 (1990-03-01)
The present study has validated kinetically a convenient method to measure tolbutamide hydroxylation capacity in human beings by use of urinary metabolic ratios. The known in vivo and in vitro inhibitory properties of sulfaphenazole were used to convert control phase
Yu Fen Zheng et al.
Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association, 68, 117-127 (2014-03-19)
We evaluated the potential of BST204, a purified dry extract of ginseng, to inhibit or induce human liver cytochrome P450 enzymes (CYPs) and UDP-glucuronosyltransferases (UGTs) in vitro to assess its safety. In vitro drug interactions of four bioactive ginsenosides of
Kim D Mooiman et al.
The Journal of pharmacy and pharmacology, 66(9), 1339-1346 (2014-04-16)
The aim of this study is to establish the inhibitory effects of 14 commonly used complementary and alternative medicines (CAM) on the metabolism of cytochrome P450 2C9 (CYP2C9) substrates 7-methoxy-4-trifluoromethyl coumarine (MFC) and tolbutamide. CYP2C9 is important for the metabolism
Yue Yu et al.
Xenobiotica; the fate of foreign compounds in biological systems, 45(6), 481-487 (2014-12-17)
1. We aimed to investigate the regulatory effects of Guanxinning injection (GXNI) on activities of cytochrome P1A2 (CYP1A2), CYP2C11, CYP2D1 and CYP3A1/2 by probe drugs in rats in vivo and in vitro. 2. GXNI-treated and blank control groups were administered
L L Hansen et al.
Therapeutic drug monitoring, 21(6), 664-671 (1999-12-22)
An isocratic, high-performance liquid chromatography method has been developed for simultaneous determination of the oral antidiabetic tolbutamide and two of its metabolites, 4-hydroxytolbutamide and carboxytolbutamide, in human plasma and urine. The method was based on simple one-step liquid-liquid extraction with
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